The present invention relates to 1,2,3,5,6,7,8,8a-octahydro-5,5,8a-trimethyl-(8a.beta.)-6-isoquinolineamine derivatives, which inhibit the biosynthesis of cholesterol, and especially of epoxysqualene cyclase, in mammals and fungi, to their method of preparation and to their use in therapeutics as hypocholesterolemics, hypolipidemics, antiatheromatous agents and antifungal agents.
Various compounds which inhibit the different enzymes involved in the biosynthesis of cholesterol, and especially of squalene epoxidase and epoxysqualene cyclase, are already known.
Numerous studies have stressed the importance and advantage of these products in the normalization of the cholesterol level and in the antifungal sphere by virtue of their capacity to inhibit the biosynthesis of ergosterol.
For example, patent application EP-A-468434 describes 4-hydroxypiperidine ethers or thioethers which inhibit epoxysqualene cyclase.
Likewise, patent applications EP-A-468457 and EP-A-420116 describe .beta.-methyl-4-piperidineethanol derivatives and alkyl-4-piperidinol compounds as squalene epoxidase inhibitors, said derivatives and compounds being useful as antiatheromatous agents and antifungal agents.
These compounds also include decalin and azadecalin derivatives such as those described for example in international patent application WO-A-89/08450 and patent U.S. Pat. No. A-5084461, which are useful as hypocholesterolemics and antifungal agents.
None of these documents of the prior art either describes or suggests 1,2,3,5,6,7,8,8a-octahydro-5,5,8a-trimethyl-(8a.beta.)-6-isoquinolineamine derivatives useful as inhibitors of the biosynthesis of cholesterol, and especially of epoxysqualene cyclase.